Antineuroinflammatory Activities and Neurotoxicological Assessment of Curcumin Loaded Solid Lipid Nanoparticles on LPS-Stimulated BV-2 Microglia Cell Models.

Govindarajan Karthivashan,Shinyoung Park,Dong-Kug Choi,Vishnu Revuri,Prakash Ramalingam,Palanivel Ganesan,Byungwook Kim,Joon Kim,Young Ko

doi:10.3390/molecules24061170

Abstract

Curcumin, which is a potential antineuroinflammatory and neuroprotective compound, exhibits poor bioavailability in brain cells due to its difficulty in crossing the blood–brain barrier and its rapid metabolism during circulation, which decreases its efficacy in treating chronic neuroinflammatory diseases in the central nervous system. The bioavailability and potential of curcumin can be improved by using a nanodelivery system, which includes solid lipid nanoparticles. Curcumin-loaded solid lipid nanoparticles (SLCN) were efficiently developed to have a particle size of about 86 nm and do not exhibit any toxicity in the endothelial brain cells. Furthermore, the curcumin-loaded solid lipid nanoparticles (SLCN) were studied to assess their efficacy in BV-2 microglial cells against LPS-induced neuroinflammation. The SLCN showed a higher inhibition of nitric oxide (NO) production compared to conventional curcumin in a dose-dependent manner. Similarly, the mRNA and proinflammatory cytokine levels were also reduced in a dose-dependent manner when compared to those with free curcumin. Thus, SLCN could be a potential delivery system for curcumin to treat microglia-mediated neuroinflammation.

Highlights

Neurodegenerative diseases, such as Parkinson’s disease (PD) or Alzheimer’s disease, are age-related chronic illnesses that are characterized by the loss of neurons and activation of microglia in brain cells [1,2]
The particle size of the solid lipid nanoparticles nanoparticles (SLCN) was slightly higher compared to that of solid lipid nanoparticles (SLN), which means that the addition of curcumin slightly increased the particle size of the SLCN
The particle size was found to be lower than 100 nm and this could facilitate a higher bioavailability of curcumin to the cells

Summary

Introduction

Neurodegenerative diseases, such as Parkinson’s disease (PD) or Alzheimer’s disease, are age-related chronic illnesses that are characterized by the loss of neurons and activation of microglia in brain cells [1,2]. Neuroinflammation leads to the activation of microglia and results in a higher production of inflammatory markers, including nitric oxide, TNF-α, IL-1β, and IL-6 [4,5,6,7]. The suppression of inflammatory markers using natural phytoextracts is in great demand for delaying neuroinflammation and its related diseases. Curcumin is a major bioactive compound that is found in turmeric powder and it is used in traditional Indian and Chinese medicine due to its various health enhancing effects to treat the inflammation associated with chronic diseases [12,13,14,15,16]. To improve the properties and biological activity, novel lipid-based delivery vehicles are in greater demand [22], such as solid lipid nanoparticles (SLN)

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